A Successful Application of Phosphazene Base P2-tBu to [11C]ABP688 Radiosynthesis in Fully Automated Synthesis Module

초록

[11C]ABP688 is the radioligand widely used for metabotropic glutamate subtype 5 (mGluR5) imaging in positron emission tomography (PET). The successful production of [11C]ABP688 in commercial automated synthesis module with hindered strong organic base was achieved. I compared 1,8-bis(tetramethylguanidino)naphthalene (TMGN), tert-butylimino-tri(pyrrolidino)phosphorane (BTPP), P2-tBu, P4-tBu, and NaH as a base for C-11 methylation of oxime and found P2-tBu would be a suitable alternative for the conventional inorganic bases (NaH or NaOH). Considering the GMP application, P2-tBu can provide compatibility with automated synthesizer and the resulting reliable synthesis. Three batches of the optimized condition for [11C]ABP688 synthesis were examined for quality assurance. © 2020 Korean Chemical Society, Seoul & Wiley-VCH GmbH

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